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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
2
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pubmed:dateCreated |
2006-12-15
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pubmed:abstractText |
The synthesis of N-arylamide phosphonates and related arylether and arylamine analogues provided potent, subtype-selective agonists and antagonists of the five known sphingosine 1-phosphate (S1P) receptors (S1P(1-5)). To this end, the syntheses of phosphoserine mimetics-selectively protected and optically active phosphonoserines-are described. In vitro binding assays showed that the implementation of phosphonates as phosphate mimetics provided compounds with similar receptor binding affinities as compared to their phosphate precursors. meta-substituted arylamide phosphonates were discovered to be antagonists of the S1P(1) and S1P(3) receptors. When administered to mice, an antagonist blocked the lymphopenia evoked by a S1P receptor agonist and caused capillary leakage in both lung and kidney.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-10956203,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-10982820,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-11119867,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-12790117,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-12816425,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-12946838,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-12969317,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-14505636,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-14737169,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-15149705,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-15307751,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-15341948,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-15497998,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-15590668,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-15598563,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-16093248,
http://linkedlifedata.com/resource/pubmed/commentcorrection/17113298-16829954
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Jan
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pubmed:issn |
0968-0896
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
663-77
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pubmed:dateRevised |
2010-12-3
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pubmed:meshHeading |
pubmed-meshheading:17113298-Animals,
pubmed-meshheading:17113298-Capillary Permeability,
pubmed-meshheading:17113298-Cell Line,
pubmed-meshheading:17113298-Guanosine Triphosphate,
pubmed-meshheading:17113298-Indicators and Reagents,
pubmed-meshheading:17113298-Lymphopenia,
pubmed-meshheading:17113298-Magnetic Resonance Spectroscopy,
pubmed-meshheading:17113298-Mice,
pubmed-meshheading:17113298-Mice, Inbred C57BL,
pubmed-meshheading:17113298-Molecular Conformation,
pubmed-meshheading:17113298-Optical Rotation,
pubmed-meshheading:17113298-Phosphonic Acids,
pubmed-meshheading:17113298-Receptors, Lysosphingolipid,
pubmed-meshheading:17113298-Tissue Distribution
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pubmed:year |
2007
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pubmed:articleTitle |
Synthesis and biological evaluation of gamma-aminophosphonates as potent, subtype-selective sphingosine 1-phosphate receptor agonists and antagonists.
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pubmed:affiliation |
Department of Chemistry, University of Virginia, McCormick Road, PO Box 400319, Charlottesville, VA 22904, USA. ff2185@columbia.edu
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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